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公开(公告)号:US20190031599A1
公开(公告)日:2019-01-31
申请号:US16072296
申请日:2017-01-24
发明人: Anne Goldby , Gemma Liwicki , Stephen Mack , Martin Teall , Katy White
IPC分类号: C07C233/41 , C07C233/23 , A61P25/30 , A61P25/18 , A61P27/16
摘要: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4a and R4b are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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公开(公告)号:US09950989B2
公开(公告)日:2018-04-24
申请号:US15118696
申请日:2015-02-13
申请人: TOA EIYO LTD.
发明人: Hidekazu Masaki , Masayuki Kageyama
IPC分类号: C07C247/14 , C07D207/335 , C07D277/28 , C07D307/52 , A61K31/13 , C07C223/04 , C07C271/24 , C07D333/20 , C07D333/22 , C07D333/32 , C07C233/41 , C07C233/79
CPC分类号: C07C223/04 , C07B2200/07 , C07C233/41 , C07C233/79 , C07C247/14 , C07C271/24 , C07C2601/14 , C07C2601/16 , C07D207/335 , C07D277/28 , C07D307/46 , C07D307/52 , C07D333/20 , C07D333/22 , C07D333/32
摘要: Provided is a novel compound having an excellent suppression effect against arrhythmia including atrial fibrillation and being useful as a pharmaceutical product without antiviral effect. Disclosed is a compound represented by the following General Formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof (in the formula, the dotted line portion represents a single bond or a double bond; R1 represents an optionally substituted C1-6 alkyl group; Q represents an oxygen atom, a sulfur atom, or NR5; R2 represents —(C═O)—R6, —CHR6R7, or —CH2OR8; and R3 and R4, which may be identical or different, each represent an amino group, an azide group, or —X—R9, with the proviso that any one of R3 and R4 is an amino group).
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公开(公告)号:US09868695B2
公开(公告)日:2018-01-16
申请号:US15519054
申请日:2015-10-14
发明人: Ram A. Vishwakarma , Sandip B. Bharate , Ajay Kumar , Baljinder Singh , Ashok Kumar , Shashi Bhushan , Abid Hamid , Prashant Joshi , Santosh K. Guru , Suresh Kumar , Aashiq Hussain , Asif K. Qazi , Sonali S. Bharate , Parduman Sharma , Ajit K. Saxena , Dilip M. Mondhe , Girish Mahajan , Zahoor Wani
IPC分类号: C07C233/41 , C07C231/12 , A61K31/165
CPC分类号: C07C233/41 , A61K31/165 , C07C231/12 , C07C2603/34
摘要: The present invention relates to the compounds of formula I wherein R is as herein described. The present invention particularly relates to synthesis and antiproliferative activity of 10-substituted colchicinoids. Compounds of the invention can be used for prevention or in the treatment of cancer disease.
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公开(公告)号:US20170304332A1
公开(公告)日:2017-10-26
申请号:US15648250
申请日:2017-07-12
发明人: Alaric J. Dyckman , T.G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC分类号: A61K31/695 , C07F9/6553 , C07F9/655 , C07F9/6509 , C07F9/6503 , C07F9/62 , C07F9/572 , C07F9/54 , C07F9/117 , C07F9/09 , C07F7/08 , C07D333/16 , C07D319/20 , C07D311/76 , C07D311/58 , C07D309/12 , C07D309/06 , C07D305/08 , C07D277/24 , C07D241/12 , C07D241/04 , C07D239/26 , C07D231/20 , C07D231/12 , C07D217/24 , C07D215/14 , C07D215/12 , C07D213/70 , C07D213/69 , C07D213/38 , C07D213/32 , C07D209/46 , C07C323/29 , C07C323/25 , C07C321/28 , C07C321/22 , C07C321/16 , C07C317/32 , C07C317/28 , C07C275/26 , C07C271/34 , C07C251/54 , C07C251/52 , C07C251/50 , C07C251/44 , C07C251/42 , C07C251/38 , C07C235/46 , C07C233/65 , C07C233/41 , C07C219/24 , C07C217/74 , C07C217/58 , C07C217/52 , C07C215/42 , A61K31/661 , A61K31/505 , A61K31/4965 , A61K31/47 , A61K31/4409 , A61K31/4406 , A61K31/4402 , A61K31/44 , A61K31/426 , A61K31/4174 , A61K31/415 , A61K31/381 , A61K31/352 , A61K31/351 , A61K31/337 , A61K31/27 , A61K31/24 , A61K31/222 , A61K31/17 , A61K31/166 , A61K31/165 , A61K31/15 , A61K31/137 , A61K31/135 , C07C2601/04 , C07C2601/08 , C07C2603/74 , C07C2602/10 , C07C2601/02
CPC分类号: A61K31/695 , A61K31/135 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661 , C07B2200/05 , C07C215/42 , C07C217/52 , C07C217/58 , C07C217/74 , C07C219/24 , C07C233/41 , C07C233/65 , C07C235/46 , C07C251/38 , C07C251/42 , C07C251/44 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C275/26 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07C323/25 , C07C323/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/10 , C07C2603/74 , C07D209/46 , C07D213/32 , C07D213/38 , C07D213/69 , C07D213/70 , C07D215/12 , C07D215/14 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/04 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F7/081 , C07F9/091 , C07F9/117 , C07F9/5442 , C07F9/5728 , C07F9/62 , C07F9/65031 , C07F9/650952 , C07F9/65522 , C07F9/655345
摘要: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号:US09770459B2
公开(公告)日:2017-09-26
申请号:US15337843
申请日:2016-10-28
发明人: Alaric J. Dyckman , T.G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC分类号: C07D217/00 , A61K31/695 , C07C215/42 , C07C217/52 , C07C217/58 , C07C219/24 , C07C233/41 , C07C233/65 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07D213/32 , C07D213/69 , C07D213/70 , C07D215/12 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F7/08 , C07F9/117 , C07F9/62 , C07F9/6503 , C07F9/6509 , C07F9/655 , C07F9/6553 , A61K31/135 , C07D215/14 , C07D241/04 , C07C323/29 , C07C251/38 , C07C251/42 , C07C251/44 , C07D209/46 , C07D213/38 , C07C275/26 , C07C217/74 , C07C323/25 , C07C235/46 , C07F9/54 , C07F9/572 , C07F9/09 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661
CPC分类号: A61K31/695 , A61K31/135 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661 , C07B2200/05 , C07C215/42 , C07C217/52 , C07C217/58 , C07C217/74 , C07C219/24 , C07C233/41 , C07C233/65 , C07C235/46 , C07C251/38 , C07C251/42 , C07C251/44 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C275/26 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07C323/25 , C07C323/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/10 , C07C2603/74 , C07D209/46 , C07D213/32 , C07D213/38 , C07D213/69 , C07D213/70 , C07D215/12 , C07D215/14 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/04 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F7/081 , C07F9/091 , C07F9/117 , C07F9/5442 , C07F9/5728 , C07F9/62 , C07F9/65031 , C07F9/650952 , C07F9/65522 , C07F9/655345
摘要: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号:US09724316B2
公开(公告)日:2017-08-08
申请号:US15262852
申请日:2016-09-12
发明人: Kevin Duane Bunker
IPC分类号: C07C233/52 , C07C217/52 , C07C233/06 , C07C233/41 , C07C235/74 , A61K31/13 , A61K31/16 , A61K31/216 , A61K31/222 , A61K31/235 , A61K45/06 , C07C233/23 , A61K31/14 , A61K31/215 , A61K31/22 , C07C211/62 , A61K9/00 , A61K31/221 , A61K31/24 , A61K31/133 , C07C233/63
CPC分类号: A61K31/16 , A61K9/0014 , A61K9/0019 , A61K31/13 , A61K31/133 , A61K31/14 , A61K31/215 , A61K31/216 , A61K31/22 , A61K31/221 , A61K31/235 , A61K31/24 , A61K45/06 , C07C211/62 , C07C217/52 , C07C233/06 , C07C233/23 , C07C233/41 , C07C233/52 , C07C233/63 , C07C235/74 , C07C2602/38
摘要: Analgesic compounds for treatment of pain or fever that include a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering a compound described herein.
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公开(公告)号:US09580386B2
公开(公告)日:2017-02-28
申请号:US14459540
申请日:2014-08-14
申请人: GRÜNENTHAL GMBH
发明人: Bert Nolte , Wolfgang Schröder , Klaus Linz , Werner Englberger , Hans Schick , Heinz Graubaum , Birgit Braun , Sigrid Ozegowski , József Bálint , Helmut Sonnenschein
IPC分类号: C07C211/00 , C07D209/20 , C07C211/40 , C07C215/14 , C07C215/42 , C07C217/74 , C07C223/04 , C07C229/16 , C07C233/36 , C07C233/40 , C07C233/41 , C07C233/62 , C07C233/79 , C07C235/54 , C07C237/06 , C07C275/24 , C07C311/07 , C07C311/18 , C07D209/12 , C07D209/14 , C07D211/62 , C07D213/12 , C07D213/82 , C07D231/14 , C07D251/54 , C07D295/135 , C07D309/08 , C07D333/20 , C07D403/08 , C07D409/08 , A61K31/135 , A61K45/06 , A61K31/136 , A61K31/165 , A61K31/18 , A61K31/404 , A61K31/53 , A61K31/5377 , C07C211/54 , C07C237/24 , C07C311/37 , C07D251/48
CPC分类号: C07D209/20 , A61K31/135 , A61K31/136 , A61K31/165 , A61K31/18 , A61K31/404 , A61K31/53 , A61K31/5377 , A61K45/06 , C07C211/40 , C07C211/54 , C07C215/14 , C07C215/42 , C07C217/74 , C07C223/04 , C07C229/16 , C07C233/36 , C07C233/40 , C07C233/41 , C07C233/62 , C07C233/79 , C07C235/54 , C07C237/06 , C07C237/24 , C07C275/24 , C07C311/07 , C07C311/18 , C07C311/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D209/12 , C07D209/14 , C07D211/62 , C07D213/12 , C07D213/82 , C07D231/14 , C07D251/48 , C07D251/54 , C07D295/135 , C07D309/08 , C07D333/20 , C07D403/08 , C07D409/08
摘要: The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
摘要翻译: 本发明涉及对μ-阿片受体和ORL1-受体具有亲和力的化合物,其生产方法,含有这些化合物的药物以及这些化合物用于治疗疼痛和其它病症的用途。
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公开(公告)号:US20170050919A1
公开(公告)日:2017-02-23
申请号:US15118696
申请日:2015-02-13
申请人: TOA EIYO LTD.
发明人: Hidekazu MASAKI , Masayuki KAGEYAMA
IPC分类号: C07C223/04 , C07D307/52 , C07C233/41 , C07D277/28 , C07C233/79 , C07D333/22 , C07D207/335
CPC分类号: C07C223/04 , C07B2200/07 , C07C233/41 , C07C233/79 , C07C247/14 , C07C271/24 , C07C2601/14 , C07C2601/16 , C07D207/335 , C07D277/28 , C07D307/46 , C07D307/52 , C07D333/20 , C07D333/22 , C07D333/32
摘要: Provided is a novel compound having an excellent suppression effect against arrhythmia including atrial fibrillation and being useful as a pharmaceutical product without antiviral effect. Disclosed is a compound represented by the following General Formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof (in the formula, the dotted line portion represents a single bond or a double bond; R1 represents an optionally substituted C1-6 alkyl group; Q represents an oxygen atom, a sulfur atom, or NR5; R2 represents —(C═O)—R6, —CHR6R7, or —CH2OR8; and R3 and R4, which may be identical or different, each represent an amino group, an azide group, or —X—R9, with the proviso that any one of R3 and R4 is an amino group).
摘要翻译: 提供一种具有优异的抑制心律失常抑制作用的新型化合物,其可用作无抗病毒作用的药物。 公开了由以下通式(I)表示的化合物,其药学上可接受的盐或其溶剂合物(在该式中,虚线部分表示单键或双键; R 1表示任选取代的C 1 -6烷基; Q表示氧原子,硫原子或NR 5; R 2表示 - (C = O)-R 6,-CHR 6 R 7或-CH 2 OR 8; R 3和R 4可以相同或不同,各自表示氨基,叠氮基或-XR 9,条件是R 3和R 4中的任一个为氨基)。
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公开(公告)号:US09487494B2
公开(公告)日:2016-11-08
申请号:US12744137
申请日:2008-11-20
IPC分类号: C07D295/182 , C07C211/35 , C07C211/36 , C07C211/48 , C07C215/28 , C07C217/52 , C07C217/74 , C07C233/05 , C07C233/41 , C07C237/24 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/40 , C07C239/14 , C07C255/03 , C07C255/32 , C07C255/50 , C07C257/18 , C07C259/10 , C07C259/18 , C07C271/44 , C07C309/15 , C07C311/05 , C07C311/08 , C07C311/37 , C07C311/51 , C07C317/32 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/80 , C07D231/12 , C07D231/40 , C07D233/61 , C07D233/90 , C07D263/22 , C07D271/06 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/192 , C07D295/195 , C07D295/26 , C07D305/08 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/79 , C07D309/10 , C07D319/18 , C07D333/38 , C07D333/40 , C07D333/58 , C07D413/04 , C07D413/06 , C07D417/06
CPC分类号: C07D295/182 , C07C211/35 , C07C211/36 , C07C211/48 , C07C215/28 , C07C217/52 , C07C217/74 , C07C233/05 , C07C233/41 , C07C237/24 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/40 , C07C239/14 , C07C255/03 , C07C255/32 , C07C255/50 , C07C257/18 , C07C259/10 , C07C259/18 , C07C271/44 , C07C309/15 , C07C311/05 , C07C311/08 , C07C311/37 , C07C311/51 , C07C317/32 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/80 , C07D231/12 , C07D231/40 , C07D233/61 , C07D233/90 , C07D263/22 , C07D271/06 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/192 , C07D295/195 , C07D295/26 , C07D305/08 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/79 , C07D309/10 , C07D319/18 , C07D333/38 , C07D333/40 , C07D333/58 , C07D413/04 , C07D413/06 , C07D417/06
摘要: The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
摘要翻译: 本发明涉及新的环烃化合物及其衍生物,其制备方法,用作药物的所述化合物,用于治疗的所述化合物,包含所述化合物的药物组合物,涉及用所述化合物治疗疾病的方法 ,以及所述化合物在制备药物中的用途。
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公开(公告)号:US09447026B2
公开(公告)日:2016-09-20
申请号:US14439636
申请日:2014-03-06
发明人: Kevin Duane Bunker
IPC分类号: C07C233/52 , C07C217/52 , C07C233/06 , C07C233/23 , C07C233/41 , C07C235/74 , A61K31/13 , A61K31/16 , A61K31/216 , A61K31/222 , A61K31/235 , A61K45/06 , A61K31/14 , A61K31/215 , A61K31/22 , C07C211/62
CPC分类号: A61K31/16 , A61K9/0014 , A61K9/0019 , A61K31/13 , A61K31/133 , A61K31/14 , A61K31/215 , A61K31/216 , A61K31/22 , A61K31/221 , A61K31/235 , A61K31/24 , A61K45/06 , C07C211/62 , C07C217/52 , C07C233/06 , C07C233/23 , C07C233/41 , C07C233/52 , C07C233/63 , C07C235/74 , C07C2602/38
摘要: Analgesic compounds for treatment of pain or fever that include a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering a compound described herein.
摘要翻译: 用于治疗疼痛或发热的止痛化合物,其包括与胺连接的双环戊烷部分,化合物与阿片类止痛药的组合,以及通过施用本文所述的化合物治疗疼痛或发热的方法。
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